JP5543982B2 - Copdの処置に有用な5−ピラゾリル−2−ピリドン誘導体のトシル酸塩 - Google Patents
Copdの処置に有用な5−ピラゾリル−2−ピリドン誘導体のトシル酸塩 Download PDFInfo
- Publication number
- JP5543982B2 JP5543982B2 JP2011550649A JP2011550649A JP5543982B2 JP 5543982 B2 JP5543982 B2 JP 5543982B2 JP 2011550649 A JP2011550649 A JP 2011550649A JP 2011550649 A JP2011550649 A JP 2011550649A JP 5543982 B2 JP5543982 B2 JP 5543982B2
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- tosylate
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- methyl
- pharmaceutical composition
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- DLKGCHGAEQGFEV-UHFFFAOYSA-N CC(C(C1)C1(Cc1cc(C(F)(F)F)ccc1)C(C(C(O)=O)=C1)=O)=C1I Chemical compound CC(C(C1)C1(Cc1cc(C(F)(F)F)ccc1)C(C(C(O)=O)=C1)=O)=C1I DLKGCHGAEQGFEV-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Inorganic Chemistry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15409909P | 2009-02-20 | 2009-02-20 | |
| US61/154,099 | 2009-02-20 | ||
| PCT/GB2010/050271 WO2010094964A1 (en) | 2009-02-20 | 2010-02-18 | Tosylate salt of a 5-pyrazolyl-2-pyridone derivative, useful in the treatment of copd |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012518623A JP2012518623A (ja) | 2012-08-16 |
| JP5543982B2 true JP5543982B2 (ja) | 2014-07-09 |
Family
ID=42046174
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011550649A Active JP5543982B2 (ja) | 2009-02-20 | 2010-02-18 | Copdの処置に有用な5−ピラゾリル−2−ピリドン誘導体のトシル酸塩 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US8232296B2 (pt) |
| EP (1) | EP2398792B1 (pt) |
| JP (1) | JP5543982B2 (pt) |
| KR (1) | KR20110127158A (pt) |
| CN (1) | CN102405219B (pt) |
| AR (1) | AR075523A1 (pt) |
| AU (1) | AU2010215269B2 (pt) |
| BR (1) | BRPI1008396B8 (pt) |
| CA (1) | CA2752319C (pt) |
| ES (1) | ES2469916T3 (pt) |
| MX (1) | MX2011008389A (pt) |
| RU (1) | RU2526038C2 (pt) |
| TW (1) | TW201036957A (pt) |
| UY (1) | UY32461A (pt) |
| WO (1) | WO2010094964A1 (pt) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0302486D0 (sv) * | 2003-09-18 | 2003-09-18 | Astrazeneca Ab | Novel compounds |
| TW200808763A (en) * | 2006-05-08 | 2008-02-16 | Astrazeneca Ab | Novel compounds I |
| TW200808771A (en) * | 2006-05-08 | 2008-02-16 | Astrazeneca Ab | Novel compounds II |
| WO2009061271A1 (en) * | 2007-11-06 | 2009-05-14 | Astrazeneca Ab | Some 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase |
| EP2671614A1 (en) * | 2007-12-21 | 2013-12-11 | University of Rochester | Molecular Targets for Treatment of Inflammation |
| TW201036957A (en) | 2009-02-20 | 2010-10-16 | Astrazeneca Ab | Novel salt 628 |
| CA2773618A1 (en) * | 2009-10-02 | 2011-04-07 | Astrazeneca Ab | 2-pyridone compounds used as inhibitors of neutrophil elastase |
| US9475041B2 (en) | 2012-04-24 | 2016-10-25 | Basf Se | Zeolitic materials and methods for their preparation using alkenyltrialkylammonium compounds |
| US20140057920A1 (en) | 2012-08-23 | 2014-02-27 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
| US9102624B2 (en) | 2012-08-23 | 2015-08-11 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
| US20140057926A1 (en) | 2012-08-23 | 2014-02-27 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
| US9744526B2 (en) * | 2012-09-26 | 2017-08-29 | Dalian Institute Of Chemical Physics, Chinese Academy Of Sciences | SAPO-34 molecular sieve and method for preparing the same |
| KR101652209B1 (ko) * | 2012-09-26 | 2016-08-29 | 달리안 인스티튜트 오브 케미컬 피직스, 차이니즈 아카데미 오브 사이언시즈 | Sapo-34 분자체 및 그 합성 방법 |
| ES2634020T3 (es) * | 2013-03-06 | 2017-09-26 | Novartis Ag | Formulaciones de compuestos orgánicos |
| RU2542100C1 (ru) * | 2013-12-24 | 2015-02-20 | Федеральное государственное бюджетное учреждение науки Институт химии растворов им. Г.А. Крестова Российской Академии Наук (ИХС РАН) | Сокристаллическая форма теофиллина с дифлунисалом или диклофенаком |
| US9221807B2 (en) * | 2014-02-21 | 2015-12-29 | Boehringer Ingelheim International Gmbh | Substituted pyridones and pyrazinones and their use as inhibitors of neutrophil elastase activity |
| WO2016128917A1 (en) * | 2015-02-12 | 2016-08-18 | Basf Se | Process for the preparation of a dealuminated zeolitic material having the bea framework structure |
| US20160257573A1 (en) * | 2015-03-03 | 2016-09-08 | Uop Llc | High surface area pentasil zeolite and process for making same |
| CN109890385B (zh) * | 2016-10-28 | 2022-08-02 | 阿斯利康(瑞典)有限公司 | (1r,2r)-2-[4-(3-甲基-1h-吡唑-5-基)苯甲酰基]-n-(4-氧代-4,5,6,7-四氢吡唑并[1,5-a]吡嗪-3-基)环己烷甲酰胺的结晶形式 |
| CN114650819A (zh) * | 2019-09-17 | 2022-06-21 | 美莱奥生物制药第四有限公司 | 用于治疗移植物排斥、闭塞性细支气管炎综合征和移植物抗宿主病的阿维来司他 |
| CN112851643B (zh) * | 2019-11-28 | 2024-01-16 | 广东东阳光药业股份有限公司 | 嘧啶苯甲酰胺化合物的盐酸盐及其用途 |
| WO2021209740A1 (en) | 2020-04-16 | 2021-10-21 | Mereo Biopharma 4 Limited | Methods involving neutrophil elastase inhibitor alvelestat for treating coronavirus infection |
| CN114075135B (zh) * | 2020-08-10 | 2024-06-11 | 上海润石医药科技有限公司 | 含邻氨基吡啶炔基的化合物的盐及其制备方法和应用 |
| AU2022214610A1 (en) * | 2021-01-27 | 2023-07-27 | Intra-Cellular Therapies, Inc. | Salt crystals |
| EP4419102A1 (en) | 2021-10-20 | 2024-08-28 | Mereo Biopharma 4 Limited | Neutrophil elastase inhibitors for use in the treatment of fibrosis |
| WO2023115795A1 (zh) * | 2021-12-23 | 2023-06-29 | 深圳安泰维生物医药有限公司 | 一种核苷类化合物的晶型 |
| WO2025078838A1 (en) | 2023-10-11 | 2025-04-17 | Mereo Biopharma 4 Limited | Alvelestat and alpha- 1 antitrypsin for treating respiratory disorders |
| WO2025133628A1 (en) | 2023-12-21 | 2025-06-26 | Mereo Biopharma 4 Limited | Use of alvelestat in specific patients |
| GB202319953D0 (en) | 2023-12-22 | 2024-02-07 | Mereo Biopharma 4 Ltd | Tablet formulations involving alvelestat |
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| FR2358891A1 (fr) * | 1976-07-22 | 1978-02-17 | Yamanouchi Pharma Co Ltd | Composes heterocycliques contenant un azote, utilise comme agents analgesiques et anti-inflammatoires |
| DE2706977A1 (de) * | 1977-02-18 | 1978-08-24 | Hoechst Ag | Benzoesaeuren und deren derivate sowie verfahren zu ihrer herstellung |
| EP0008864A1 (en) | 1978-08-15 | 1980-03-19 | FISONS plc | Pyridopyrazine and quinoxaline derivatives, processes for their preparation, and pharmaceutical compositions containing them |
| JPH02152966A (ja) | 1988-12-05 | 1990-06-12 | Otsuka Pharmaceut Co Ltd | 4−ヒドロキシカルボスチリル誘導体 |
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| PE20040950A1 (es) | 2003-02-14 | 2005-01-01 | Theravance Inc | DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS |
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| SE0302487D0 (sv) * | 2003-09-18 | 2003-09-18 | Astrazeneca Ab | Novel compounds |
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| CA2557271C (en) | 2004-02-26 | 2012-08-21 | Bayer Healthcare Ag | 1,4-diaryl-dihydropyrimidin-2-ones and their use as human neutrophil elastase inhibitors |
| DE102004024453A1 (de) | 2004-05-14 | 2006-01-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue langwirksame Bronchodilatoren zur Behandlung von Atemwegserkrankungen |
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| BRPI0807004A2 (pt) | 2007-02-07 | 2014-04-15 | Argenta Discovery Ltd | Sal |
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| KR20090110353A (ko) | 2007-02-15 | 2009-10-21 | 아젠터 디스커버리 리미티드 | M3 무스카린 수용체로서의 헤테로시클릭 유도체 |
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| WO2009058076A1 (en) | 2007-11-02 | 2009-05-07 | Astrazeneca Ab | 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase |
| WO2009061271A1 (en) | 2007-11-06 | 2009-05-14 | Astrazeneca Ab | Some 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase |
| HRP20120968T1 (hr) | 2008-02-06 | 2013-01-31 | Astrazeneca Ab | Spojevi |
| EA017627B1 (ru) | 2008-05-13 | 2013-01-30 | Астразенека Аб | Хинуклидиновые производные в качестве антагонистов мускаринового м3 рецептора |
| GB0811099D0 (en) | 2008-06-17 | 2008-07-23 | Astrazeneca Ab | New combination 376 |
| US7862384B2 (en) * | 2008-07-07 | 2011-01-04 | Myers Kelly H | Repair adapter for a modular plug |
| TW201036957A (en) | 2009-02-20 | 2010-10-16 | Astrazeneca Ab | Novel salt 628 |
-
2010
- 2010-02-12 TW TW099104696A patent/TW201036957A/zh unknown
- 2010-02-16 US US12/706,313 patent/US8232296B2/en active Active
- 2010-02-18 MX MX2011008389A patent/MX2011008389A/es active IP Right Grant
- 2010-02-18 ES ES10705178.1T patent/ES2469916T3/es active Active
- 2010-02-18 CN CN2010800174198A patent/CN102405219B/zh active Active
- 2010-02-18 RU RU2011135627/04A patent/RU2526038C2/ru active
- 2010-02-18 EP EP10705178.1A patent/EP2398792B1/en active Active
- 2010-02-18 KR KR1020117019327A patent/KR20110127158A/ko not_active Ceased
- 2010-02-18 WO PCT/GB2010/050271 patent/WO2010094964A1/en not_active Ceased
- 2010-02-18 CA CA2752319A patent/CA2752319C/en active Active
- 2010-02-18 AU AU2010215269A patent/AU2010215269B2/en active Active
- 2010-02-18 AR ARP100100488A patent/AR075523A1/es unknown
- 2010-02-18 BR BRPI1008396A patent/BRPI1008396B8/pt active IP Right Grant
- 2010-02-18 JP JP2011550649A patent/JP5543982B2/ja active Active
- 2010-02-19 UY UY0001032461A patent/UY32461A/es unknown
-
2012
- 2012-06-27 US US13/534,687 patent/US20120269872A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP2398792A1 (en) | 2011-12-28 |
| JP2012518623A (ja) | 2012-08-16 |
| EP2398792B1 (en) | 2014-04-09 |
| RU2526038C2 (ru) | 2014-08-20 |
| UY32461A (es) | 2010-09-30 |
| AR075523A1 (es) | 2011-04-06 |
| AU2010215269B2 (en) | 2013-06-27 |
| CN102405219A (zh) | 2012-04-04 |
| BRPI1008396B8 (pt) | 2021-05-25 |
| WO2010094964A1 (en) | 2010-08-26 |
| CA2752319A1 (en) | 2010-08-26 |
| CN102405219B (zh) | 2013-11-06 |
| KR20110127158A (ko) | 2011-11-24 |
| CA2752319C (en) | 2016-10-04 |
| US8232296B2 (en) | 2012-07-31 |
| ES2469916T3 (es) | 2014-06-20 |
| US20120269872A1 (en) | 2012-10-25 |
| BRPI1008396B1 (pt) | 2020-11-10 |
| MX2011008389A (es) | 2011-09-01 |
| HK1162498A1 (en) | 2012-08-31 |
| TW201036957A (en) | 2010-10-16 |
| BRPI1008396A2 (pt) | 2017-06-27 |
| US20100216843A1 (en) | 2010-08-26 |
| AU2010215269A1 (en) | 2011-08-25 |
| RU2011135627A (ru) | 2013-03-27 |
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